Oculoselective Drugs and Prodrugs
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Accused Products
Abstract
Compounds of the following formula are disclosed: wherein R1 and R2 are each independently H, W, or a phenoxyl protecting group; and R4 is H or W, provided that at least one of R1, R2, and R4 is W; R3 is hydrogen, straight chain or branched C1-C10 alkyl, cycloalkyl, amino, C1-C10 alkoxy, —NHC(═O)Ra, or —C(═O)N(H)Ra; Ra is alkyl, aryl, or heterocyclyl; Z is -0-, —O(C═O)—, or NH(C═O)—, wherein when Z is -0-, R5 is H, straight chain or branched C1-C10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C1-C10 alkyl, CI—Clo alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolsdinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with CI—Clo alkyl, C1-C10 alkoxy, or halo; and W is: wherein each R6 is independently H, straight chain or branched C1-C10 alkyl, or straight chain or branched C1-C10 alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is —O(C═O)—, R5 is straight chain or branched C1-C10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C1-C10 alkyl, CI—CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C1-C10 alkyl, C1-C10 alkoxy, or halo; and W is:, wherein each R6 is independently H, straight chain or branched CI—C to alkyl, or straight chain or branched C,—C to alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is —NH(C═O)—, R5 is straight chain or branched C1-C10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C1-C10 alkyl, CI—CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, & oxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C1-C10 alkyl, C1-C10 alkoxy, or halo; and W is: wherein each R6 is independently H, straight chain or branched C1-C to alkyl, or straight chain or branched C,—Clo alkoxyalkyl. Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions, are also disclosed.
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Citations
62 Claims
- 1. A compound of Formula I:
- 20. A compound of Formula II:
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46. A process for producing a compound of formula IIIa:
Specification